187840-69-3Relevant academic research and scientific papers
5-(4'-Substituted-2'-nitroanilino)-1,2,3-triazoles as new potential potassium channel activators. I
Biagi, Giuliana,Calderone, Vincenzo,Giorgi, Irene,Livi, Oreste,Scartoni, Valerio,Baragatti, Barbara,Martinotti, Enrica
, p. 715 - 720 (2000)
By the hypothesised correlation with the large conductance Ca++- activated potassium channel (BK(Ca)) openers NS 004 and NS 1619, bearing a benzimidazolone ring, a series of new 5-(4'-substituted-2'-nitroanilino)- 1,2,3-triazoles were synthesised and tested on in vitro isolated vascular preparation. The compounds were prepared starting from the appropriately substituted 2-nitro-phenylazides by 1,3-dipolar cycloaddition reaction to cyanoacetamide and following Dimroth isomerisation of the corresponding 1- arylsubstituted-5-amino-1,2,3-triazoles. The analogous 5-(4'-substituted-2'- amino-anilino)-1,2,3-triazoles were also prepared to assess the role of the nitro group in the pharmacophoric model. Almost all the nitro compounds showed a vasorelaxant activity on endothelium-denuded rat aortic rings with a potency comparable to that recorded for the reference compound NS 1619. Such a vasorelaxing activity was significantly reduced by the increase of the level of membrane depolarisation and by the potassium channel blocker 4- aminopyridine with a pharmacodynamic behaviour consistent with a potassium channel activation. (C) 2000 Editions scientifiques et medicales Elsevier SAS.
New 4-(Benzotriazol-1-yl)-1,2,3-Triazole Derivatives
Biagi, Gialiana,Giorgi, Irene,Livi, Oreste,Scartoni, Valerio,Velo, Silvia,Barili, Pier Luigi
, p. 1847 - 1853 (2007/10/03)
A new 4-(benzotriazol-1-yl)-l,2,3-triazole structure was obtained by the diazotization reaction of either of 1-(2-aminophenyl)-4-carboxamido-5-amino-1H-1,2,3-triazole (1c) or of the corresponding Dimroth isomer 1d. It underwent some common reactions to ev
